Synthesis, characterization, molecular docking and cholinesterase inhibition studies of new thiazole-hydrazinyl derivatives
نویسندگان
چکیده
Alzheimer hastalığı (AD), beyinde asetilkolin üreten veya kullanan kolinerjik hücrelerin yıkımı kaybından kaynaklanmaktadır. Bundan dolayı, AD için ana tedavi stratejisi beyindeki seviyesini arttırmaktır.
 Bu çalışmada, kolinesteraz inhibitörleri olarak yeni tiyazol-hidrazinil türevlerinin sentezi gerçekleştirilmiştir. Sentezlenen bileşiklerin yapısı 1H-NMR ve 13C-NMR verileri ile aydınlatılmıştır. hedef asetilkolinesteraz (AChE) butirilkolinesteraz (BChE) inhibitör etkileri Ellman yöntemi kullanılarak değerlendirilmiştir. Moleküler doking çalışması Autodock Vina yapılmıştır. 
 bütün AChE karşı düşük etkinlik sergilediği bulunmuştur. bileşikler arasından sadece bileşik 3j seçici BuChE inhibe ettiği Dokingden elde edilen verilere göre 3j, aktif sitesinde 10.0 kcal/mol etkileşim enerjisi Trp82 anahtar pi-pi staked etkileşimleri oluşturmuştur. Sonuç olarak, bu çalışma hastalığının tedavisinde inhibitörü ajan geliştirmede yol göstericidir.
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ژورنال
عنوان ژورنال: Bal?kesir Üniversitesi Fen Bilimleri Enstitüsü Dergisi
سال: 2023
ISSN: ['1301-7985', '2536-5142']
DOI: https://doi.org/10.25092/baunfbed.1113229